Discovery of R-142086 as a factor Xa (FXa) inhibitor: syntheses and structure-activity relationships of cinnamyl derivatives.

@article{Noguchi2009DiscoveryOR,
  title={Discovery of R-142086 as a factor Xa (FXa) inhibitor: syntheses and structure-activity relationships of cinnamyl derivatives.},
  author={T. Noguchi and N. Tanaka and T. Nishimata and R. Goto and M. Hayakawa and A. Sugidachi and T. Ogawa and Y. Niitsu and F. Asai and T. Ishizuka and Koichi Fujimoto},
  journal={Chemical & pharmaceutical bulletin},
  year={2009},
  volume={57 1},
  pages={
          22-33
        }
}
  • T. Noguchi, N. Tanaka, +8 authors Koichi Fujimoto
  • Published 2009
  • Medicine, Chemistry
  • Chemical & pharmaceutical bulletin
  • To develop a novel and effective anticoagulant with potent and selective factor Xa (FXa) inhibitory activity, a new series of cinnamyl derivatives with enhanced lipophilicity and prodrug forms were synthesized and their biological activities were evaluated. As a result, we found that cinnamyl derivative (N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid dihydrochloride (26d, R-142086) with a fluorine atom on the… CONTINUE READING
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